Sixty-six percent of adults in the United States are overweight or obese. Obesity is a medical condition in which excess body fat has accumulated to the extent that it may have an adverse effect on a person's health leading to reduced life expectancy. Obesity is an epidemic in the United States and in other developed countries as nearly one-third of the population is obese. Further, obesity is on the rise as food is abundant and physical activity is optional.
Obesity has many serious long-term consequences and it is the second leading cause of preventable deaths in the United States. It is associated with many diseases, particularly heart disease, type 2 diabetes, breathing difficulties during sleep, certain types of cancer and osteoarthritis. Obesity is most commonly caused by a combination of excessive dietary calories, lack of physical activity and genetic susceptibility.
Billions of dollars are spent each year on weight control and obesity treatments. In addition, approximately $45 billion is spent each year on treating the diseases associated with obesity. Furthermore, businesses suffer an estimated $20 billion loss in productivity each year from absence due to illness caused by obesity.
The primary treatment for obesity is dieting and physical exercise. If this fails, anti-obesity drugs may be taken to reduce appetite or inhibit fat absorption. In severe cases, surgery is performed or an intragastric balloon is placed to reduce stomach volume and or bowel length, leading to earlier satiation and reduced ability to absorb nutrients from food.
As far as anti-obesity medications, only two are currently approved by the U.S. Food and Drug Administration (“FDA”) for long term use. Orlistat (Xenical) is currently approved by the FDA and it reduces intestinal fat absorption by inhibiting pancreatic lipase. Sibutramine (Meridia) is also approved by the FDA and it acts in the brain to inhibit deactivation of the neurotransmitters norepinephrine, serotonin and dopamine thereby decreasing appetite. A third medication, Rimonabant (Acomplia), is approved in Europe and it works by blocking the endocannabinoid system. Weight loss with these drugs has been shown to be modest with the following average weight losses: Orlistat—6.4 lbs; Sibutramine—9.3 lbs; and Rimonabant—10.4 lbs.
Accordingly, there is a need to develop more effective pharmaceuticals since maintaining a healthy body weight and/or avoiding obesity can help control cholesterol, blood pressure and blood sugar which can help prevent weight-related diseases, such as heart disease, diabetes, arthritis and some cancers.
One pharmaceutical with minimal side effects that is known to the medical profession is clonidine, which is widely recognized as an antihypertensive agent that acts as an agonist on the alpha-2-adrenergic receptor and a neural receptor agonist. In general, clonidine, also referred to as 2,6-dichloro-N-2-imidazolidinyldenebenzenamine (C9H9Cl2N3), may be represented by the following chemical structure:

Another compound is fluocinolone which is known to the medical profession for reducing inflammation and/or immunological rejection of transplanted tissue. Fluocinolone in its acetonide form (C24H30F2O6) has been administered topically as a cream in connection with hand transplants. It may also be referred to as 4b,12-Difluoro-6b-glycoloyl-5-hydroxy-4a,6a,8,8-tetramethyl-4a,4b,5,6,6a,6b,9a,10,10a,10b,11,12-dodecahydro-2H-naphtho[2′,1′:4,5]indeno[1,2- d][1,3]dioxol-2-one or 6α-,9α-Difluoro-16 α-hydroxyprednisolone 16,17-acetonide.
However, to date, neither clonidine nor fluocinolone have been widely appreciated as a treatment for weight control and/or reduction or prevention of obesity. This invention is directed to effective formulations including one or both of these compounds for these applications.